Quinidine hydrobromide is an antiarrhythmic agent. Quinidine is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine hydrobromide is also a K+ channel blocker with an IC50 of 19.9 μM. Quinidine hydrobromide can be used for malaria research[1][2][3].
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity[1]. CGP 39551 shows measurable inhibitory activity at both L-[3H]-glutamate (Ki=8.4 μM)[2].
GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy[1].
Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits?GABA receptor?with?IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits Autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1[1][2][3][4].
TRPC5-IN-2 is a potent TRPC5 inhibitor (WO2019055966A2, Compound IO)[1].
ω-Conotoxin CnVIIA, a 27 amino acid neuropeptide toxin, is a N-type calcium current blocker[1].
VX-661 is a second F508del CFTR corrector and help CFTR protein reach the cell surface.
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively[1]. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase[2]. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis[3]. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway[4].
CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes[1][2].
p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
HM30181 is a potent and selective inhibitor of P-glycoprotein.
Tofogliflozin(CSG-452) hydrate is a potent and highly specific sodium/glucose cotransporter 2(SGLT2) inhibitor with Ki values of 2.9, 14.9, and 6.4 nM for human, rat, and mouse SGLT2.IC50 value: 2.9/14.9/6.4 nM(human/rat/mouse SGLT2) [1]Target: SGLT2 inhibitorin vitro: Tofogliflozin competitively inhibited SGLT2 in cells overexpressing SGLT2, and K(i) values for human, rat, and mouse SGLT2 inhibition were 2.9, 14.9, and 6.4 nM, respectively. The selectivity of tofogliflozin toward human SGLT2 versus human SGLT1, SGLT6, and sodium/myo-inositol transporter 1 was the highest among the tested SGLT2 inhibitors under clinical development [1]. tofogliflozin was catalyzed to the primary hydroxylated derivative (M4) by CYP2C18, CYP4A11 and CYP4F3B, then M4 was oxidized to M1. 3. Tofogliflozin had no induction potential on CYP1A2 and CYP3A4 [4].in vivo: A single oral gavage of tofogliflozin increased renal glucose clearance and lowered the blood glucose level in Zucker diabetic fatty rats. Tofogliflozin also improved postprandial glucose excursion in a meal tolerance test with GK rats. In db/db mice, 4-week tofogliflozin treatment reduced glycated hemoglobin and improved glucose tolerance in the oral glucose tolerance test 4 days after the final administration [1]. Tofogliflozin (400 ng/ml) induced UGE of about 2 mg/kg per min and increased EGP by 1-2 mg/kg per min, resulting in PG in the normal range [2]. Tofogliflozin suppressed plasma glucose and glycated Hb and preserved pancreatic beta-cell mass and plasma insulin levels. No improvement of glycaemic conditions or insulin level was observed with losartan treatment [3].
NMDA receptor antagonist 5 (Compound 10e) is a potent, brain permeable and non-toxic NMDA receptor antagonist. NMDA receptor antagonist 5 can be used for neurological disorder research[1].
Stearoyl-L-carnitine chloride is an endogenous long-chain acylcarnitine. Stearoyl-L-carnitine chloride is a less potent inhibitor of GlyT2. Stearoyl-L-carnitine chloride inhibits glycine responses by 16.8% at concentrations up 3 μM[1][2].
Vecuronium bromide is a nondepolarizing neuromuscular blocking agent of intermediate duration.
AZD3965 is a selective MCT1 inhibitor with a Ki of 1.6 nM, showing 6-fold selectivity over MCT2.
D-3263 is an agonist of transient receptor potential melastatin member 8 (TRPM8) with potential antineoplastic activity.
RO2959 hydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 hydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 hydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways[1][2].
YM543 free base is a potent and orally active sodium-glucose cotransporter (SGLT) 2 inhibitor. YM543 free base reduces blood glucose levels. YM543 free base can be used in research of diabetes[1][2].
NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a partial N-methyl-D-aspartate receptor (NMDAR) agonist used in the study of depression, anxiety, and other related diseases.
AUT1 is a Kv3 potassium channel modulator, with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5)[1].
CGP 37849 is a potent, competitive and orally active N-methyl-D-aspartate (NMDA) receptor antagonist. CGP 37849 is an anticonvulsant in rodents and has antidepressant and anxiolytic-like effects[1].
Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker. Target: Calcium ChannelLacidipine, a novel third-generation dihydropyridine calcium channel blocker, has been demonstrated effective for hypertension. lacidipine protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway [1]. In biological membranes deriving from rat brain tissue, lacidipine showed an activity comparable to reference antioxidant compounds like vitamin E [2]. lacidipine has some important protective effects on liver of hypertensive irradiated albino rats [3].
PK-THPP is a potent TWIK-related acid-sensitive K(+) ion channel (TASK-3 ion channel) blocker (IC50s are 35 nM and 300 nM for TASK-3 and TASK-1, respectively)[1]. PK-THPP increases breathing rate and induces respiratory alkalosis in rats[2].
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.Preparation of 2-[(4-benzyl)-1-piperidinyl)methyl]benzimidazole-5-ols as NMDA NR2B receptor antagonists for the treatment of neuropathic pain.By McCauley, James A.; Claremon, David A.; Liverton, Nigel J. From PCT Int. Appl. (2004), WO 2004048364 A1 20040610. NR2B-Selective N-Methyl-D-aspartate Antagonists: Synthesis and Evaluation of 5-Substituted BenzimidazolesBy McCauley, John A.; Theberge, Cory R.; Romano, Joseph J.; Billings, Susan B.; Anderson, Kenneth D.; Claremon, David A.; Freidinger, Roger M.; Bednar, Rodney A.; Mosser, Scott D.; Gaul, Stanley L.; et alFrom Journal of Medicinal Chemistry (2004), 47(8), 2089-2096.
UK-78282, a novel piperidine, potent and selective Kv1.3 blocker with an IC50 of 200 nM. UK-78,282 effectively suppresses human T-lymphocyte activation in vitro. UK-78,282 binds to residues at the inner surface of the channel overlapping the site of action of verapamil[1].
Quinine dihydrochloride is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine dihydrochloride is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM[1][2].
Bamaluzole is a GABA receptor agonist extracted from patent WO 2012064642 A1.
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca2+-activated K+ (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca2+ and stimulates transmitter release[1][2].